PE20130396A1 - N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQUINOLINE-3-CARBOXAMIDE DEUTERATED, SALTS AND USES OF THE SAME - Google Patents

N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQUINOLINE-3-CARBOXAMIDE DEUTERATED, SALTS AND USES OF THE SAME

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Publication number
PE20130396A1
PE20130396A1 PE2013000039A PE2013000039A PE20130396A1 PE 20130396 A1 PE20130396 A1 PE 20130396A1 PE 2013000039 A PE2013000039 A PE 2013000039A PE 2013000039 A PE2013000039 A PE 2013000039A PE 20130396 A1 PE20130396 A1 PE 20130396A1
Authority
PE
Peru
Prior art keywords
carboxamide
chloro
hydroxy
phenyl
ethyl
Prior art date
Application number
PE2013000039A
Other languages
Spanish (es)
Inventor
Victor Piryatinsky
Avital Laxer
Original Assignee
Teva Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45439026&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20130396(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Teva Pharma filed Critical Teva Pharma
Publication of PE20130396A1 publication Critical patent/PE20130396A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/465—Nicotine; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/5545—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having eight-membered rings not containing additional condensed or non-condensed nitrogen-containing 3-7 membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Abstract

SE REFIERE AL COMPUESTO N-ETIL-N-FENIL-1,2-DIHIDRO-4-HIDROXI-5-CLORO-1-METIL-2-OXOQUINOLIN-3-CARBOXAMIDA (LAQUINIMOD) ENRIQUECIDO CON DEUTERIO DE FORMULA (i), (ii) O (iii) DONDE D ES DEUTERIO. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA QUE CONTIENE A) LAQUINIMOD ENRIQUECIDO CON DEUTERIO; B) UN PORTADOR FARMACEUTICAMENTE ACEPTABLE; Y C) EL COMPUESTO 5-CLORO-4-HIDROXI-1-METIL-2-OXO-N-FENIL-1,2-DIHIDROQUINOLIN-3-CARBOXAMIDA O DES-ETIL-LAQUINIMOD EN UNA CANTIDAD MENOR DE 0.1% CON BASE EN EL PESO COMBINADO DE DICHO COMPUESTO Y LAQUINIMOD ENRIQUECIDO CON DEUTERIO. DICHO COMPUESTO SE ADMINISTRA EN UNA CANTIDAD DE 0.2MG A 2MG POR DIA SIENDO UTIL EN EL TRATAMIENTO DE ESCLEROSIS MULTIPLEREFERS TO THE COMPOUND N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQUINOLIN-3-CARBOXAMIDE (LAQUINIMOD) ENRICHED WITH DEUTERIUM FORMULA (i), ( ii) OR (iii) WHERE D IS DEUTERIO. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION CONTAINING A) LAQUINIMOD ENRICHED WITH DEUTERIUM; B) A PHARMACEUTICALLY ACCEPTABLE CARRIER; AND C) THE COMPOUND 5-CHLORO-4-HYDROXY-1-METHYL-2-OXO-N-PHENYL-1,2-DIHYDROQUINOLIN-3-CARBOXAMIDE OR DES-ETHYL-LAQUINIMOD IN AN AMOUNT OF LESS THAN 0.1% BASED ON COMBINED WEIGHT OF SAID COMPOUND AND LAQUINIMOD ENRICHED WITH DEUTERIUM. SAID COMPOUND IS ADMINISTERED IN AN AMOUNT OF 0.2MG TO 2MG PER DAY BEING USEFUL IN THE TREATMENT OF MULTIPLE SCLEROSIS

PE2013000039A 2010-07-09 2011-07-08 N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQUINOLINE-3-CARBOXAMIDE DEUTERATED, SALTS AND USES OF THE SAME PE20130396A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US39929710P 2010-07-09 2010-07-09

Publications (1)

Publication Number Publication Date
PE20130396A1 true PE20130396A1 (en) 2013-04-19

Family

ID=45439026

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013000039A PE20130396A1 (en) 2010-07-09 2011-07-08 N-ETHYL-N-PHENYL-1,2-DIHYDRO-4-HYDROXY-5-CHLORO-1-METHYL-2-OXOQUINOLINE-3-CARBOXAMIDE DEUTERATED, SALTS AND USES OF THE SAME

Country Status (19)

Country Link
US (3) US8580819B2 (en)
EP (2) EP3213636A1 (en)
JP (2) JP2013535437A (en)
KR (1) KR20130092558A (en)
CN (2) CN102984939A (en)
AR (1) AR082150A1 (en)
AU (1) AU2011274496B2 (en)
BR (1) BR112013000599A2 (en)
CA (1) CA2804986A1 (en)
CL (1) CL2013000063A1 (en)
EA (1) EA025377B1 (en)
IL (1) IL251600A0 (en)
MX (1) MX2013000333A (en)
NZ (1) NZ606587A (en)
PE (1) PE20130396A1 (en)
SG (2) SG10201505236YA (en)
UY (1) UY33504A (en)
WO (1) WO2012006538A1 (en)
ZA (1) ZA201300956B (en)

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EP3213636A1 (en) 2010-07-09 2017-09-06 Teva Pharmaceutical Industries, Ltd. Deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, salts and uses thereof
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PE20140872A1 (en) 2010-12-07 2014-08-09 Teva Pharma USE OF LAQUINIMOD TO REDUCE FATIGUE, IMPROVE FUNCTIONAL STATUS AND IMPROVE QUALITY OF LIFE IN PATIENTS WITH MULTIPLE SCLEROSIS

Also Published As

Publication number Publication date
EP3213636A1 (en) 2017-09-06
CL2013000063A1 (en) 2013-05-03
US20120010238A1 (en) 2012-01-12
JP2017014238A (en) 2017-01-19
EP2597954A1 (en) 2013-06-05
AR082150A1 (en) 2012-11-14
WO2012006538A1 (en) 2012-01-12
ZA201300956B (en) 2014-04-30
MX2013000333A (en) 2013-02-26
US9102620B2 (en) 2015-08-11
NZ606587A (en) 2015-03-27
EA025377B1 (en) 2016-12-30
SG10201505236YA (en) 2015-08-28
JP2013535437A (en) 2013-09-12
AU2011274496B2 (en) 2016-03-10
BR112013000599A2 (en) 2016-07-05
SG186948A1 (en) 2013-02-28
WO2012006538A8 (en) 2013-05-23
US20140051723A1 (en) 2014-02-20
AU2011274496A1 (en) 2013-02-28
UY33504A (en) 2012-02-29
US20140343096A1 (en) 2014-11-20
EP2597954A4 (en) 2014-01-01
KR20130092558A (en) 2013-08-20
EA201390081A1 (en) 2013-07-30
IL251600A0 (en) 2017-06-29
CN104610144A (en) 2015-05-13
US8580819B2 (en) 2013-11-12
CA2804986A1 (en) 2012-01-12
CN102984939A (en) 2013-03-20

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